Guanfacine-¹⁵N¹³,¹³C₂  (Synonyms: 胍法辛-¹⁵N₃,¹³C₂)

Guanfacine-¹⁵N₃,¹³C₂ is ¹⁵N and ¹³C labeled Guanfacine (HY-17416A). Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD)^[1][2][3].

氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Guanfacine enhances PFC working memory function in aged monkeys and improves impulse control in monkeys performing a delayed discounting task^[2][4].
Guanfacine improves cognitive performance when infused directly into the rat or monkey PFC^[2][4].
Guanfacine blocks 2A receptors in the monkey dIPFC markedly impairs working memory, behavioral inhibition and greatly reduces persistent neuronal firing^[2][4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

251.06

C₇¹³C₂H₉Cl₂¹⁵N₃O

29110-47-2

胍法辛-¹⁵N₃,¹³C₂；胍法新-¹⁵N₃,¹³C₂；氯苯乙胍-¹⁵N₃,¹³C₂

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. Amy F T Arnsten, et al. Guanfacine for the treatment of cognitive disorders: a century of discoveries at Yale. Yale J Biol Med. 2012 Mar;85(1):45-58. Epub 2012 Mar 29.  [Content Brief]

  [3]. P. A. Van Zwieten, et al. The pharmacology of centrally acting antihypertensive drugs. Br J Clin Pharmacol. 1983; 15(Suppl 4): 455S–462S.

  [4]. Min Wang, et al. Alpha2A-adrenoceptors strengthen working memory networks by inhibiting cAMP-HCN channel signaling in prefrontal cortex. Cell. 2007 Apr 20;129(2):397-410.  [Content Brief]